<i>GPR142</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

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GPR142

Target not currently curated in GtoImmuPdb

Target id: 132

Nomenclature: GPR142

Family: Class A Orphans

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 462 17q23 GPR142 G protein-coupled receptor 142 1-2
Mouse 7 365 11 E2 Gpr142 G protein-coupled receptor 142 1-2
Rat 7 - 10q32.2 Gpr142 G protein-coupled receptor 142
Previous and Unofficial Names
KIF19 | AXOR103 | G-protein coupled receptor PGR2
Database Links
Specialist databases
GPCRDB gp142_human (Hs), gp142_mouse (Mm)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Parameter Reference
compound 33 [Toda et al., 2013] Hs Agonist 7.7 pEC50 3
pEC50 7.7 (EC50 2.2x10-8 M) [3]
Agonist Comments
The high identity of 50% between GPR142 and GPR139 is suggestive of shared ligands [2].
Tissue Distribution
Brain (intense labeling of hippocampus, dentate gyrus, cerebral cortex, medial thalamic nuclei, anterior hypothalamic nuclei), thymus, liver, cartilage
Species:  Mouse
Technique:  In situ hybridization
References:  2
Spleen, liver, kidney, testis, brain
Species:  Mouse
Technique:  Multi-tissue cDNA panel (PCR)
References:  2
Tissue Distribution Comments
Embryonic expression of GPR142 suggests the receptor may play a role in brain, bone and blood formation [2].
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  R86H
Global MAF (%):  1
Subpopulation MAF (%):  ASN: 3
Minor allele count:  A=0.007/16
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  H132D
Global MAF (%):  3
Subpopulation MAF (%):  AFR|AMR: 12|3
Minor allele count:  C=0.032/70
SNP accession: 
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  R124Q
Global MAF (%):  1
Subpopulation MAF (%):  AFR: 3
Minor allele count:  A=0.006/14
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
Validation:  1000 Genomes, Frequency

References

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1. Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB. (2003) Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives. FEBS Lett., 554 (3): 381-8. [PMID:14623098]

2. Süsens U, Hermans-Borgmeyer I, Urny J, Schaller HC. (2006) Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development. Neuropharmacology, 50 (4): 512-20. [PMID:16378626]

3. Toda N, Hao X, Ogawa Y, Oda K, Yu M, Fu Z, Chen Y, Kim Y, Lizarzaburu M, Lively S et al.. (2013) Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes. ACS Med Chem Lett, 4 (8): 790-4. [PMID:24900747]

Contributors

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How to cite this page

Stephen P.H. Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner, Anthony P. Davenport, Satoru Eguchi, Anthony Harmar, Nick Holliday, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Wen Chiy Liew, Amy E. Monaghan, Chido Mpamhanga, Richard Neubig, Adam J. Pawson, Jean-Philippe Pin, Joanna L. Sharman, Michael Spedding, Eliot Spindel, Leigh Stoddart, Laura Storjohann, Walter (Wally) Thomas, Kalyan Tirupula, Patrick Vanderheyden.
Class A Orphans: GPR142. Last modified on 13/07/2018. Accessed on 19/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=132.